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Literature summary for 1.14.14.18 extracted from

  • Rahman, M.N.; Vlahakis, J.Z.; Szarek, W.A.; Nakatsu, K.; Jia, Z.
    X-ray crystal structure of human heme oxygenase-1 in complex with 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone: a common binding mode for imidazole-based heme oxygenase-1 inhibitors (2008), J. Med. Chem., 51, 5943-5952.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
truncated, soluble version of HO-1 that contains 233 amino acids expressed from plasmid HO1-t233/pBace in Escherichia coli DH5alpha Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
HO-1 in complex with 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone, by sitting-drop vapor diffusion method, at room temperature, to 1.5 A resolution. Overall structure of the HO-1-inhibitor complex is very similar to that of the native heme-conjugated HO-1, being mostly alpha-helical with the heme sandwiched between the proximal and distal helices. The inhibitor binds to the HO-1 distal pocket such that the imidazolyl moiety coordinates with heme iron while the adamantyl group is stabilized by a hydrophobic binding pocket. Distal helix flexibility, coupled with shifts in proximal residues and heme, acts to expand the distal pocket, thus accommodating the bulky inhibitor without displacing heme. Inhibitor binding effectively displaces the catalytically critical distal water ligand Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Fe2+
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09601
-
-

Purification (Commentary)

Purification (Comment) Organism
on anion-exchange column Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
heme + electron donor + O2
-
Homo sapiens biliverdin + Fe2+ + CO + oxidized electron donor + H2O
-
?

Synonyms

Synonyms Comment Organism
heme oxygenase-1
-
Homo sapiens
HO-1
-
Homo sapiens